Lipid Lowering Drugs Flashcards
What is the target cholesterol?
less than or equal to 4 mmol/L - 5mmol/l when you have CVD risk
non-HDL - less than or equal to 2.5 mmol/L
HDL - less than or equal to 1.8 mmol/L
What is the role of lipid lowering drugs?
Target levels of cholesterol and lipids in patients with a high CV risk
Examples of lipid-lowering drugs
Statins
Ezetimide
Fibrates
Bile acid-binding resins
Nicotinic acid
Omega-3-acid ethyl esters (fish oil derivatives)
What is the main lipid-lowering effects?
Reduction of circulating LDL
Modest increases in plasma HDL
Name the fungal derived statins (type 1)
Pravastatin, Simvastatin
Name the synthetically derived statins (type 2)
Atorvastatin, Rosuvastatin, Fluvastatin
Describe the clinical uses of statins
Secondary prevention of CHD
Primary prevention of CHD in patents with other risk factors:
- diabetes
- chronic kidney disease
in familiar hypercholesterolaemia
What should statins be cautioned/contraindicated?
Caution in patients with:
- Liver disease
- Hypothyrodism
Contradictions - pregnancy as cholesterol is important in the formation of the baby
Name some CV benefits of statins
Improvement of endothelial function
Anti-inflammatory - inhibition of prenylation of small GTPase like Rha,Rac, cdc42
Anti-thrombotic and Antiplatelets effects
Increase in vasodilation - inhibition of RhoA-ROCK pathway by preventing post-translation prenylation of RhoA
Increase in neovascularization of ischaemic tissue (e.g. coronary circulation)
Name the common ADRs with statins
Asthenia - physical weakness
Muscle pain (myalgia)
Nausea, dizziness, headache
Constipation, diarrhoea
Flatulence and GI discomfort
Thrombocytopenia - reduced number of white blood cells
Name the RARE and VERY RARE side effects
Rare:
Myopathies
- Myositis - muscle inflammation
- Rhabdomyolysis - muscle breakdown
Very Rare:
Hepatitis
Intestinal Lung Disease
Name the RARE and VERY RARE side effects
Rare:
Myopathies
- Myositis - muscle inflammation
- Rhabdomyolysis - muscle breakdown
Very Rare:
Hepatitis
Intestinal Lung Disease
Name which drugs which inhibit CYP3A4 leading to increased statin levels
Anti-fungal (itraconazole)
Antibiotics (erythromycin, clarithromycin)
CCBs (verapamil, dilitazem)
Immunosuppressants (cyclosporins)
Grapefruit juice